Zhan-Guo Gao, M.D., Ph.D.

Photo of Zhan-Guo Gao.
Scientific Focus Areas: Biomedical Engineering and Biophysics, Cancer Biology, Immunology, Microbiology and Infectious Diseases, Molecular Pharmacology

Publications

A selection of recent and significant publications can be viewed below.

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin.
Gao ZG, Jacobson KA.
Biochem Pharmacol (2016 May 1) 107:59-66. Abstract/Full Text
UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation.
Gao ZG, Ding Y, Jacobson KA.
Biochem Pharmacol (2010 Mar 15) 79:873-9. Abstract/Full Text
Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
Tosh DK, Chinn M, Ivanov AA, Klutz AM, Gao ZG, Jacobson KA.
J Med Chem (2009 Dec 10) 52:7580-92. Abstract/Full Text
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.
Choi WJ, Lee HW, Kim HO, Chinn M, Gao ZG, Patel A, Jacobson KA, Moon HR, Jung YH, Jeong LS.
Bioorg Med Chem (2009 Dec 1) 17:8003-11. Abstract/Full Text
PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G protein-coupled receptors.
Kim Y, Hechler B, Gao ZG, Gachet C, Jacobson KA.
Bioconjug Chem (2009 Oct 21) 20:1888-98. Abstract/Full Text
Synthesis and pharmacological characterization of [(125)I]MRS1898, a high-affinity, selective radioligand for the rat A(3) adenosine receptor.
Gao ZG, Teng B, Wu H, Joshi BV, Griffiths GL, Jacobson KA.
Purinergic Signal (2009 Mar) 5:31-7. Abstract/Full Text
Application of the functionalized congener approach to dendrimer-based signaling agents acting through A(2A) adenosine receptors.
Kim Y, Klutz AM, Hechler B, Gao ZG, Gachet C, Jacobson KA.
Purinergic Signal (2009 Mar) 5:39-50. Abstract/Full Text
The A3 adenosine receptor agonist CF502 inhibits the PI3K, PKB/Akt and NF-kappaB signaling pathway in synoviocytes from rheumatoid arthritis patients and in adjuvant-induced arthritis rats.
Ochaion A, Bar-Yehuda S, Cohen S, Amital H, Jacobson KA, Joshi BV, Gao ZG, Barer F, Patoka R, Del Valle L, Perez-Liz G, Fishman P.
Biochem Pharmacol (2008 Aug 15) 76:482-94. Abstract/Full Text
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Melman A, Gao ZG, Kumar D, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.
Bioorg Med Chem Lett (2008 May 1) 18:2813-9. Abstract/Full Text
Synthesis of 3'-acetamidoadenosine derivatives as potential A3 adenosine receptor agonists.
Chun MW, Choi SW, Kang TK, Choi WJ, Kim HO, Gao ZG, Jacobson KA, Jeong LS.
Nucleosides Nucleotides Nucleic Acids (2008 Apr) 27:408-20. Abstract/Full Text
Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways.
Gao ZG, Jacobson KA.
Pharmacol Res (2008 Apr) 57:303-11. Abstract/Full Text
Caged agonist of P2Y1 and P2Y12 receptors for light-directed facilitation of platelet aggregation.
Gao ZG, Hechler B, Besada P, Gachet C, Jacobson KA.
Biochem Pharmacol (2008 Mar 15) 75:1341-7. Abstract/Full Text
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.
Jeong LS, Lee HW, Kim HO, Tosh DK, Pal S, Choi WJ, Gao ZG, Patel AR, Williams W, Jacobson KA, Kim HD.
Bioorg Med Chem Lett (2008 Mar 1) 18:1612-6. Abstract/Full Text
Emerging adenosine receptor agonists.
Gao ZG, Jacobson KA.
Expert Opin Emerg Drugs (2007 Sep) 12:479-92. Abstract/Full Text
Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides.
Palaniappan KK, Gao ZG, Ivanov AA, Greaves R, Adachi H, Besada P, Kim HO, Kim AY, Choe SA, Jeong LS, Jacobson KA.
Biochemistry (2007 Jun 26) 46:7437-48. Abstract/Full Text
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
Adachi H, Palaniappan KK, Ivanov AA, Bergman N, Gao ZG, Jacobson KA.
J Med Chem (2007 Apr 19) 50:1810-27. Abstract/Full Text
Neoceptors: reengineering GPCRs to recognize tailored ligands.
Jacobson KA, Gao ZG, Liang BT.
Trends Pharmacol Sci (2007 Mar) 28:111-6. Abstract/Full Text
Stereoselective synthesis of 1'-functionalized-4'-thionucleosides.
Jeong LS, Gunaga P, Kim HO, Tosh DK, Lee HW, Choe SA, Moon HR, Gao ZG, Jacobson KA, Chun MW.
Nucleosides Nucleotides Nucleic Acids (2007) 26:1011-4. Abstract/Full Text
Design, synthesis, and anti-tumor activity of 4'-thionucleosides as potent and selective agonists at the human A3 adenosine receptor.
Jeong LS, Lee HW, Kim HO, Jung JY, Gunaga P, Lee SK, Lee EJ, Chun MW, Gao ZG, Jacobson KA, Moon HR.
Nucleosides Nucleotides Nucleic Acids (2007) 26:1565-8. Abstract/Full Text
Synthesis of N6-substituted 3'-ureidoadenosine derivatives as highly potent agonists at the mutant A3 adenosine receptor.
Jeong LS, Choe SA, Kim AY, Kim HO, Gao ZG, Jacobson KA, Chun MW, Moon HR.
Nucleosides Nucleotides Nucleic Acids (2007) 26:717-9. Abstract/Full Text
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
Cosyn L, Palaniappan KK, Kim SK, Duong HT, Gao ZG, Jacobson KA, Van Calenbergh S.
J Med Chem (2006 Dec 14) 49:7373-83. Abstract/Full Text
Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor.
Kim SK, Gao ZG, Jeong LS, Jacobson KA.
J Mol Graph Model (2006 Dec) 25:562-77. Abstract/Full Text
Regulation of death and survival in astrocytes by ADP activating P2Y1 and P2Y12 receptors.
Mamedova LK, Gao ZG, Jacobson KA.
Biochem Pharmacol (2006 Oct 16) 72:1031-41. Abstract/Full Text
Design, synthesis, and biological activity of N6-substituted-4'-thioadenosines at the human A3 adenosine receptor.
Jeong LS, Lee HW, Kim HO, Jung JY, Gao ZG, Duong HT, Rao S, Jacobson KA, Shin DH, Lee JA, Gunaga P, Lee SK, Jin DZ, Chun MW, Moon HR.
Bioorg Med Chem (2006 Jul 15) 14:4718-30. Abstract/Full Text
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Göblyös A, Gao ZG, Brussee J, Connestari R, Santiago SN, Ye K, Ijzerman AP, Jacobson KA.
J Med Chem (2006 Jun 1) 49:3354-61. Abstract/Full Text
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
Gao ZG, Duong HT, Sonina T, Kim SK, Van Rompaey P, Van Calenbergh S, Mamedova L, Kim HO, Kim MJ, Kim AY, Liang BT, Jeong LS, Jacobson KA.
J Med Chem (2006 May 4) 49:2689-702. Abstract/Full Text
Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands.
Cosyn L, Gao ZG, Van Rompaey P, Lu C, Jacobson KA, Van Calenbergh S.
Bioorg Med Chem (2006 Mar 1) 14:1403-12. Abstract/Full Text
Progress in the pursuit of therapeutic adenosine receptor antagonists.
Moro S, Gao ZG, Jacobson KA, Spalluto G.
Med Res Rev (2006 Mar) 26:131-59. Abstract/Full Text
Adenosine receptors as therapeutic targets.
Jacobson KA, Gao ZG.
Nat Rev Drug Discov (2006 Mar) 5:247-64. Abstract/Full Text
Keynote review: allosterism in membrane receptors.
Gao ZG, Jacobson KA.
Drug Discov Today (2006 Mar) 11:191-202. Abstract/Full Text
Structure activity and molecular modeling analyses of ribose- and base-modified uridine 5'-triphosphate analogues at the human P2Y2 and P2Y4 receptors.
Jacobson KA, Costanzi S, Ivanov AA, Tchilibon S, Besada P, Gao ZG, Maddileti S, Harden TK.
Biochem Pharmacol (2006 Feb 14) 71:540-9. Abstract/Full Text
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.
Gao ZG, Joshi BV, Klutz AM, Kim SK, Lee HW, Kim HO, Jeong LS, Jacobson KA.
Bioorg Med Chem Lett (2006 Feb) 16:596-601. Abstract/Full Text
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
Jeong LS, Lee HW, Jacobson KA, Kim HO, Shin DH, Lee JA, Gao ZG, Lu C, Duong HT, Gunaga P, Lee SK, Jin DZ, Chun MW, Moon HR.
J Med Chem (2006 Jan 12) 49:273-81. Abstract/Full Text
Action of nucleosides and nucleotides at 7 transmembrane-spanning receptors.
Jacobson KA, Costanzi S, Kim SK, Roh E, Joshi BV, Tchilibon S, Duong HT, Gao ZG.
Nucleosides Nucleotides Nucleic Acids (2006) 25:1425-36. Abstract/Full Text
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.
Jacobson KA, Gao ZG, Tchilibon S, Duong HT, Joshi BV, Sonin D, Liang BT.
J Med Chem (2005 Dec 29) 48:8103-7. Abstract/Full Text
CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors.
Mamedova L, Capra V, Accomazzo MR, Gao ZG, Ferrario S, Fumagalli M, Abbracchio MP, Rovati GE, Jacobson KA.
Biochem Pharmacol (2005 Dec 19) 71:115-25. Abstract/Full Text
New 8-substituted xanthiene derivatives as potent bronchodilators.
Berk B, Akgün H, Erol K, Sirmagül B, Gao ZG, Jacobson KA.
Farmaco (2005 Nov-Dec) 60:974-80. Abstract/Full Text
Signaling of the Human P2Y(1) Receptor Measured by a Yeast Growth Assay with Comparisons to Assays of Phospholipase C and Calcium Mobilization in 1321N1 Human Astrocytoma Cells.
Niebauer RT, Gao ZG, Li B, Wess J, Jacobson KA.
Purinergic Signal (2005 Sep) 1:241-7. Abstract/Full Text
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
Perreira M, Jiang JK, Klutz AM, Gao ZG, Shainberg A, Lu C, Thomas CJ, Jacobson KA.
J Med Chem (2005 Jul 28) 48:4910-8. Abstract/Full Text
Activation of Th1 and Tc1 cell adenosine A2A receptors directly inhibits IL-2 secretion in vitro and IL-2-driven expansion in vivo.
Erdmann AA, Gao ZG, Jung U, Foley J, Borenstein T, Jacobson KA, Fowler DH.
Blood (2005 Jun 15) 105:4707-14. Abstract/Full Text
Allosteric modulation of the adenosine family of receptors.
Gao ZG, Kim SK, Ijzerman AP, Jacobson KA.
Mini Rev Med Chem (2005 Jun) 5:545-53. Abstract/Full Text
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
Tchilibon S, Joshi BV, Kim SK, Duong HT, Gao ZG, Jacobson KA.
J Med Chem (2005 Mar 24) 48:1745-58. Abstract/Full Text
Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety.
Van Rompaey P, Jacobson KA, Gross AS, Gao ZG, Van Calenbergh S.
Bioorg Med Chem (2005 Feb 15) 13:973-83. Abstract/Full Text
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
Jacobson KA, Ohno M, Duong HT, Kim SK, Tchilibon S, Cesnek M, Holý A, Gao ZG.
Chem Biol (2005 Feb) 12:237-47. Abstract/Full Text
D-4'-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptor.
Lee HW, Shin DH, Jeong JY, Kim HO, Chun MW, Melman N, Gao ZG, Jacobson KA, Jeong LS.
Nucleosides Nucleotides Nucleic Acids (2005) 24:607-9. Abstract/Full Text
Synthesis of 3'-ureidoadenosine analogues and their binding affinity to the A3 adenosine receptor.
Chun MW, Lee HW, Kim AY, Kim MJ, Kim HO, Gao ZG, Jacobson KA, Jeong LS.
Nucleosides Nucleotides Nucleic Acids (2005) 24:1119-21. Abstract/Full Text
Nucleoside modification and concerted mutagenesis of the human A3 adenosine receptor to probe interactions between the 2-position of adenosine analogs and Gln167 in the second extracellular loop.
Duong HT, Gao ZG, Jacobson KA.
Nucleosides Nucleotides Nucleic Acids (2005) 24:1507-17. Abstract/Full Text
Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands.
Tchilibon S, Kim SK, Gao ZG, Harris BA, Blaustein JB, Gross AS, Duong HT, Melman N, Jacobson KA.
Bioorg Med Chem (2004 May 1) 12:2021-34. Abstract/Full Text
Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists.
Jung KY, Kim SK, Gao ZG, Gross AS, Melman N, Jacobson KA, Kim YC.
Bioorg Med Chem (2004 Feb 1) 12:613-23. Abstract/Full Text
Partial agonists for A(3) adenosine receptors.
Gao ZG, Jacobson KA.
Curr Top Med Chem (2004) 4:855-62. Abstract/Full Text